Shopping Cart

Remove All

Your shopping cart is currently empty

Proceed to checkout Continue shopping

GSK 4027

Name: GSK 4027
Brand: TargetMol
SKU: T11495L
Rating: 4.5 (1 reviews)

Copy Product Info

😃Good

Catalog No. T11495LCas No. 2079896-25-4

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. In a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, it has a pIC50 of 7.4±0.11 for PCAF.

GSK 4027

Copy Product Info

😃Good

Catalog No. T11495LCas No. 2079896-25-4

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. In a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, it has a pIC50 of 7.4±0.11 for PCAF.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$268	35 days	35 days
5 mg	$589	35 days	35 days

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Resource Download

Product Introduction

Bioactivity

Description	GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. In a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, it has a pIC50 of 7.4±0.11 for PCAF.
Targets&IC50	PCAF:(pic50)7.4±0.11
In vitro	The selectivity of GSK 4027 against the wider bromodomain family is assessed in the BROMOscan panel (pKi of 8.9 and 8.9 for PCAF and GCN5, respectively). GSK 4027 displays equipotent activity against PCAF and GCN5 (Ki: 1.4 nM for both bromodomains). GSK 4027 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC50s of <4.3 and 5.1±0.08, respectively. Due to the encouraging measured artificial membrane permeability (500 nm/s), treatment of HEK293 cells with GSK 4027 displace full-length PCAF from histone H3.3 with little drop-off from the biochemical assay and a pIC50 7.2 (IC50 60 nM)[1].

Chemical Properties

Molecular Weight	377.28
Formula	C₁₇H₂₁BrN₄O
Cas No.	2079896-25-4
Smiles	CN1C[C@@H](C[C@@H](C1)c1ccccc1)Nc1cnn(C)c(=O)c1Br
Relative Density.	1.45 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (132.53 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6506 mL	13.2528 mL	26.5055 mL	132.5276 mL
5 mM	0.5301 mL	2.6506 mL	5.3011 mL	26.5055 mL
10 mM	0.2651 mL	1.3253 mL	2.6506 mL	13.2528 mL
20 mM	0.1325 mL	0.6626 mL	1.3253 mL	6.6264 mL
50 mM	0.0530 mL	0.2651 mL	0.5301 mL	2.6506 mL
100 mM	0.0265 mL	0.1325 mL	0.2651 mL	1.3253 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc